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Preparation method of sterile tacrolimus nano suspension eye drops

A nano-suspension, tacrolimus technology, applied in the preparation of sterile nano-suspension eye drops, the field of preparation of sterile tacrolimus nano-suspension eye drops, can solve many aseptic operation steps. , Sterile difficulty, strong eye irritation, etc.

Active Publication Date: 2016-01-27
NCPC NEW DRUG RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the patents CN104784114A and CN104382848A, the preparation method of tacrolimus suspension eye drops is respectively mentioned, wherein the prescription composition of the patent CN104784114A contains organic solvents, which are highly irritating to the eyeballs; in the patent CN104382848A, a tangential flow ultrafiltration device is used Replace the solvent to remove the residual organic solvent. The tangential flow ultrafiltration device used in this method is expensive, and the method needs to keep the tacrolimus suspension sterile. There are many aseptic operation steps, and it is difficult to make the product aseptic. Big

Method used

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  • Preparation method of sterile tacrolimus nano suspension eye drops
  • Preparation method of sterile tacrolimus nano suspension eye drops
  • Preparation method of sterile tacrolimus nano suspension eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] 1. Prescription composition

[0064] Table 1 Example 1 The composition of the prescription in the preparation of sterile tacrolimus nano-suspension eye drops

[0065]

[0066] The concentration of tacrolimus in the suspension is about 10 times that of the finished product, the volume ratio of the organic solvent (absolute ethanol) to the aqueous phase is 15:100, the weight ratio of tacrolimus to the particle size stabilizing excipient polyvinyl alcohol It is 1:1.6.

[0067] 2. Preparation process:

[0068] (1) Preparation of tacrolimus nanosuspension

[0069] Weigh the prescribed amount of tacrolimus raw material, add it into an organic solvent (absolute ethanol in this example), stir and dissolve, and use it as the organic phase. Weigh the prescribed amount of stabilizing excipients (polyvinyl alcohol in this example) into water, stir to dissolve (the water phase can be heated in a water bath at 40-60°C, which is conducive to the rapid dissolution of polyvinyl al...

Embodiment 2

[0082] prescription composition

[0083] Table 2 The composition of the prescription in the preparation of the sterile tacrolimus nano-suspension eye drops of Example 2

[0084]

[0085] The concentration of tacrolimus in the suspension is about 30 times that of the finished product, the volume ratio of the organic solvent (absolute ethanol) to the aqueous phase is 1:20, the weight of tacrolimus and the particle size stabilizing excipient polyethylene glycol The ratio is 1:10.

Embodiment 3

[0087] prescription composition

[0088] Table 3 Example 3 The composition of the prescription in the preparation of sterile tacrolimus nano-suspension eye drops

[0089]

[0090] The concentration of tacrolimus in the suspension is about 5 times that of the finished product, the volume ratio of the organic solvent (absolute ethanol) to the water phase is 1:100, and the ratio of tacrolimus and particle size stable excipient hypromellose The weight ratio is 1:20.

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Abstract

The invention relates to a method for preparing sterile tacrolimus nano suspension eye drops. The method for preparing the sterile tacrolimus nano suspension eye drops comprises the following main steps: preparing tacrolimus nano suspension by adopting a phase transfer and high pressure homogenization method; removing an organic solvent in the tacrolimus nano suspension by adopting a drying / curing technology, and stabilizing tacrolimus nano particles; sterilizing to obtain sterile tacrolimus nano particles; and finally carrying out sterile redissolution and prepackaging operation, so that the finished product is obtained. By adopting the method for preparing the sterile tacrolimus nano suspension eye drops, homogeneously dispersed sterile nano eye drops which do not contain the organic solvent can be obtained, sterile operation steps are obvious reduced, the tacrolimus nano suspension eye drops prepared by adopting the method provided by the invention is sterile and qualified, all the inspection indexes are respectively consistent with those of the original product, and especially particle size and particle size distribution are highly consistent with those of the original product.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of a sterile nano-suspension eye drop, in particular to a preparation method of a sterile tacrolimus nano-suspension eye drop. Background technique [0002] Vernal keratoconjunctivitis (VKC), also known as vernal catarrhal conjunctivitis and seasonal conjunctivitis, is a recurrent bilateral chronic ocular surface disease and is an allergic disease. VKC mainly affects children and young adults and is most common in the spring. VKC is typically characterized by giant papillae in the upper palpebral conjunctiva bilaterally, and the main symptom is persistent itching. [0003] Tacrolimus (Tacrolimus, FK506) is a new type of macrolide immunosuppressant, which belongs to calmodulin phosphatase inhibitor. Its immunosuppressive mechanism is similar to that of cyclosporine A, but the effect of inhibiting T cells is 10-100 times that of cyclosporine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/436A61P27/02
Inventor 周立明张莉徐彦孙焕茹齐志良孙莉马苗锐
Owner NCPC NEW DRUG RES & DEV
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